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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and In Vitro Evaluation of Adenosine Deaminase Resistant N-6 Aminal and Thioaminal Prodrugs of Cordycepin

Author(s): Hui-Min Chang, Jesse Oakes, Anders Olsson, Luminita Panaitescu, B. Mark Britt, Christopher M. Kearney and Robert R. Kane

Volume 2, Issue 2, 2005

Page: [133 - 136] Pages: 4

DOI: 10.2174/1570180053175151

Price: $65


Cordycepin (3;-deoxyadenosine) is a potent anti-leukemic, anti-fungal, and anti-parasitic nucleoside antibiotic. Unfortunately, the biological activity of cordycepin is attenuated by its rapid conversion to 3;-deoxyinosine by adenosine deaminase (ADA). We have synthesized a series of ADA-resistant N-aminal and N-thioaminal cordycepin derivatives, which are protected from inactivation by deamination and yet retain biological activity. These compounds are hydrolyzed at various rates to efficiently release the parent drug cordycepin, and likely serve as simple hydrolytically activated prodrugs.

Keywords: cordycepin, adenosine deaminase, leukemia, prodrug

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